PD180970_product_DataBase

Bioactivity

PD180970 is a highly potent and ATP-competitive p210Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research[1][2][3].

Invitro

PD180970 (0.5 μM; 24-96 hours) treatment causes cell death K562 cells[1].PD180970 (0.5 μM; 24-48 hours) treatment induces apoptosis of K562 cells. The result shows increase in annexin V-PI double-positive cells[1]. PD180970 inhibits tyrosine phosphorylation of p210Bcr-Abl, Gab2, and CrkL in K562 cells with IC50 values of 170 nM, 80 nM, and 80 nM, respectively. In vitro, PD180970 potently inhibits autophosphorylation of p210Bcr-Abl (IC50 of 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 of 2.2 nM)[1].The blocking Bcr-Abl kinase activity using PD180970 in the human K562 CML cell line resulted in inhibition of Stat5 DNA-binding activity with an IC50 of 5 nM[2]. Cell Viability Assay[1] Cell Line:

Name

PD180970

CAS

287204-45-9

Formula

C21H15Cl2FN4O

Molar Mass

429.27

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

PeptideDB

PD180970

CAS: 287204-45-9 F: C21H15Cl2FN4O W: 429.27